TWI704146B - 用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物 - Google Patents
用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物 Download PDFInfo
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- TWI704146B TWI704146B TW103132898A TW103132898A TWI704146B TW I704146 B TWI704146 B TW I704146B TW 103132898 A TW103132898 A TW 103132898A TW 103132898 A TW103132898 A TW 103132898A TW I704146 B TWI704146 B TW I704146B
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- 238000001195 ultra high performance liquid chromatography Methods 0.000 description 1
- 229960002703 undecylenic acid Drugs 0.000 description 1
- 229940035893 uracil Drugs 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 206010046766 uterine cancer Diseases 0.000 description 1
- ZOCKGBMQLCSHFP-KQRAQHLDSA-N valrubicin Chemical compound O([C@H]1C[C@](CC2=C(O)C=3C(=O)C4=CC=CC(OC)=C4C(=O)C=3C(O)=C21)(O)C(=O)COC(=O)CCCC)[C@H]1C[C@H](NC(=O)C(F)(F)F)[C@H](O)[C@H](C)O1 ZOCKGBMQLCSHFP-KQRAQHLDSA-N 0.000 description 1
- 229960000653 valrubicin Drugs 0.000 description 1
- 230000035899 viability Effects 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 235000019166 vitamin D Nutrition 0.000 description 1
- 239000011710 vitamin D Substances 0.000 description 1
- 150000003710 vitamin D derivatives Chemical class 0.000 description 1
- 229940046008 vitamin d Drugs 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 238000012447 xenograft mouse model Methods 0.000 description 1
- 229940004212 yondelis Drugs 0.000 description 1
- UGZADUVQMDAIAO-UHFFFAOYSA-L zinc hydroxide Chemical compound [OH-].[OH-].[Zn+2] UGZADUVQMDAIAO-UHFFFAOYSA-L 0.000 description 1
- 229940007718 zinc hydroxide Drugs 0.000 description 1
- 229910021511 zinc hydroxide Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (4)
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EP13186139 | 2013-09-26 | ||
EP13186139.5 | 2013-09-26 | ||
EP14176121.3 | 2014-07-08 | ||
EP14176121 | 2014-07-08 |
Publications (2)
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TW201602104A TW201602104A (zh) | 2016-01-16 |
TWI704146B true TWI704146B (zh) | 2020-09-11 |
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TW103132898A TWI704146B (zh) | 2013-09-26 | 2014-09-24 | 用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物 |
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US (1) | US10005773B2 (ru) |
EP (1) | EP3071566B1 (ru) |
JP (1) | JP6402179B2 (ru) |
KR (1) | KR102317334B1 (ru) |
CN (1) | CN105579451B (ru) |
AU (1) | AU2014327233B2 (ru) |
BR (1) | BR112016005914A2 (ru) |
CA (1) | CA2922753C (ru) |
EA (1) | EA029595B1 (ru) |
ES (1) | ES2804595T3 (ru) |
HK (1) | HK1224295A1 (ru) |
IL (1) | IL244706B (ru) |
MX (1) | MX2016003861A (ru) |
TW (1) | TWI704146B (ru) |
WO (1) | WO2015044267A1 (ru) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
TWI627173B (zh) | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 |
TWI704146B (zh) | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物 |
EP3209662B1 (en) | 2014-10-23 | 2019-01-09 | Janssen Pharmaceutica N.V. | New compounds as nik inhibitors |
JP6616412B2 (ja) | 2014-10-23 | 2019-12-04 | ヤンセン ファーマシューティカ エヌ.ベー. | Nik阻害剤としての新規のピラゾロピリミジン誘導体 |
US10323045B2 (en) | 2014-10-23 | 2019-06-18 | Janssen Pharmaceutica Nv | Thienopyrimidine derivatives as NIK inhibitors |
US9981962B2 (en) | 2014-10-23 | 2018-05-29 | Janssen Pharmaceutica Nv | Pyrazole derivatives as NIK inhibitors |
JP6910359B2 (ja) | 2016-01-22 | 2021-07-28 | ヤンセン ファーマシューティカ エヌ.ベー. | Nik阻害剤としての新たな置換されたシアノインドリン誘導体 |
AU2017208555B2 (en) | 2016-01-22 | 2021-03-18 | Janssen Pharmaceutica Nv | New 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
EP3478675B1 (en) * | 2016-06-30 | 2020-04-22 | Janssen Pharmaceutica NV | Heteroaromatic derivatives as nik inhibitors |
WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
CN109641894B (zh) * | 2016-08-24 | 2022-09-09 | 豪夫迈·罗氏有限公司 | 2-氮杂双环[3.1.0]己烷-3-酮衍生物及使用方法 |
WO2018037058A1 (en) | 2016-08-24 | 2018-03-01 | F. Hoffmann-La Roche Ag | 2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use |
US11254673B2 (en) | 2019-05-31 | 2022-02-22 | Janssen Pharmaceutica Nv | Small molecule inhibitors of NF-κB inducing kinase |
CN113816957B (zh) * | 2021-10-29 | 2023-04-07 | 浙江工业大学 | 4-(7-氮杂吲哚)-2-氨基嘧啶类化合物及其应用 |
Citations (2)
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WO2007058850A2 (en) * | 2005-11-10 | 2007-05-24 | Smithkline Beecham Corporation | Inhibitors of akt activity |
WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
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JP3990061B2 (ja) * | 1998-01-05 | 2007-10-10 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | プリン誘導体および糖尿病の予防・治療剤としてのアデノシンa2受容体拮抗剤 |
BRPI0510319A (pt) | 2004-04-26 | 2007-10-16 | Pfizer | inibidores da enzima integrase de hiv |
DE102008005493A1 (de) | 2008-01-22 | 2009-07-23 | Merck Patent Gmbh | 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate |
WO2010003133A2 (en) | 2008-07-03 | 2010-01-07 | Exelixis Inc. | Cdk modulators |
WO2010042337A1 (en) * | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
CN101723936B (zh) | 2008-10-27 | 2014-01-15 | 上海睿星基因技术有限公司 | 激酶抑制剂及其在药学中的用途 |
WO2011050245A1 (en) * | 2009-10-23 | 2011-04-28 | Yangbo Feng | Bicyclic heteroaryls as kinase inhibitors |
BR112013023681A2 (pt) * | 2011-03-16 | 2016-12-13 | Hoffmann La Roche | compostos de álcool propargílico 6,5-heterocíclico e uso dos mesmos |
TWI663166B (zh) * | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
TWI627173B (zh) * | 2013-09-26 | 2018-06-21 | 比利時商健生藥品公司 | 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 |
TWI704146B (zh) | 2013-09-26 | 2020-09-11 | 比利時商健生藥品公司 | 用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物 |
EP3209662B1 (en) | 2014-10-23 | 2019-01-09 | Janssen Pharmaceutica N.V. | New compounds as nik inhibitors |
US9981962B2 (en) | 2014-10-23 | 2018-05-29 | Janssen Pharmaceutica Nv | Pyrazole derivatives as NIK inhibitors |
US10323045B2 (en) | 2014-10-23 | 2019-06-18 | Janssen Pharmaceutica Nv | Thienopyrimidine derivatives as NIK inhibitors |
JP6616412B2 (ja) | 2014-10-23 | 2019-12-04 | ヤンセン ファーマシューティカ エヌ.ベー. | Nik阻害剤としての新規のピラゾロピリミジン誘導体 |
-
2014
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- 2014-09-25 MX MX2016003861A patent/MX2016003861A/es active IP Right Grant
- 2014-09-25 CA CA2922753A patent/CA2922753C/en active Active
- 2014-09-25 EA EA201690645A patent/EA029595B1/ru not_active IP Right Cessation
- 2014-09-25 KR KR1020167007899A patent/KR102317334B1/ko active IP Right Grant
- 2014-09-25 US US15/024,603 patent/US10005773B2/en active Active
- 2014-09-25 EP EP14772372.0A patent/EP3071566B1/en active Active
- 2014-09-25 AU AU2014327233A patent/AU2014327233B2/en not_active Ceased
- 2014-09-25 WO PCT/EP2014/070484 patent/WO2015044267A1/en active Application Filing
- 2014-09-25 CN CN201480052786.XA patent/CN105579451B/zh active Active
- 2014-09-25 ES ES14772372T patent/ES2804595T3/es active Active
- 2014-09-25 BR BR112016005914A patent/BR112016005914A2/pt not_active Application Discontinuation
- 2014-09-25 JP JP2016517332A patent/JP6402179B2/ja active Active
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2016
- 2016-03-22 IL IL244706A patent/IL244706B/en active IP Right Grant
- 2016-11-04 HK HK16112697.3A patent/HK1224295A1/zh not_active IP Right Cessation
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007058850A2 (en) * | 2005-11-10 | 2007-05-24 | Smithkline Beecham Corporation | Inhibitors of akt activity |
WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
Also Published As
Publication number | Publication date |
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AU2014327233B2 (en) | 2018-03-01 |
CN105579451B (zh) | 2017-10-27 |
BR112016005914A2 (pt) | 2017-08-01 |
JP2016531868A (ja) | 2016-10-13 |
CA2922753A1 (en) | 2015-04-02 |
AU2014327233A1 (en) | 2016-03-10 |
IL244706B (en) | 2021-02-28 |
CA2922753C (en) | 2021-08-17 |
EP3071566B1 (en) | 2020-04-15 |
KR102317334B1 (ko) | 2021-10-26 |
TW201602104A (zh) | 2016-01-16 |
EA201690645A1 (ru) | 2016-08-31 |
US10005773B2 (en) | 2018-06-26 |
US20160257679A1 (en) | 2016-09-08 |
ES2804595T3 (es) | 2021-02-08 |
EA029595B1 (ru) | 2018-04-30 |
EP3071566A1 (en) | 2016-09-28 |
HK1224295A1 (zh) | 2017-08-18 |
WO2015044267A1 (en) | 2015-04-02 |
JP6402179B2 (ja) | 2018-10-10 |
CN105579451A (zh) | 2016-05-11 |
MX2016003861A (es) | 2016-07-26 |
IL244706A0 (en) | 2016-04-21 |
KR20160058814A (ko) | 2016-05-25 |
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